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Compound Detail

CHEMBL553502

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COc1cc2c(cc1OC)C(c1ccnc(-n3ccc4c(OCc5cccnc5)cccc4c3=O)c1)=N[C@H](CO)C2.Cl

Basic Information

ChEMBL ID CHEMBL553502
Phase Preclinical
Structure Type MOL
InChI Key QXQATGMAYITDDO-BQAIUKQQSA-N
Parent Compound CHEMBL1194887
Active Moiety CHEMBL1194887
1
Targets
2
Activities
2
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

548.6
MW (Da)
4.13
ALogP
9
HBA
1
HBD
108.1
PSA (Ų)
0.31
QED
1
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C32H29ClN4O5
MW 585.06
Aromatic Rings 5
Heavy Atoms 41
NP-Likeness -0.37

Activity Summary

IC50 1 meas. best 9.4
Ki 1 meas. best 8.82

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Phosphodiesterase 4
CHEMBL2093863
IC50 9.4 9.4 0.4 1
Phosphodiesterase 4
CHEMBL2093863
Ki 8.82 8.82 1.5 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
12824031 10.1016/s0960-894x(03)00438-4 Phosphodiesterase 4 3
12824031 10.1016/s0960-894x(03)00438-4 Mus musculus 1

Data from ChEMBL 36 via Core Engine